Yuan Zhe-dong
2007
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Journal
Chinese Journal of Pharmaceuticals
Abstract
Darifenacin hydrobromide was synthesized from trans-4-hydroxy-L-proline by decarboxylation, N-protection, Mitsunobu reaction, condensation, deprotection, hydrolysis, salt formation and basification to give the key intermediate 3-(S)-(-)-(1-carbamoyl-1,1-diphenylmethyl)pyrrolidine, followed by condensation with 5-(2-bromoethyl)-2,3-dihydrobenzofuran and salt formation with an overall yield of about 2%.